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Pectin-silica gels as matrices for controlled drug release in gastrointestinal tract

Vityazev, Fedor V., Fedyuneva, Maiia I., Golovchenko, Victoria V., Patova, Olga A., Ipatova, Elena U., Durnev, Eugene A., Martinson, Ekaterina A., Litvinets, Sergey G.
Carbohydrate polymers 2017 v.157 pp. 9-20
Fourier transform infrared spectroscopy, absorption, calcium chloride, drug formulations, drugs, encapsulation, gastric juice, gastrointestinal system, gelation, gels, hardness, pectins, silica, sol-gel processing
The synthesis of pectin-silica gels for controlled drug release in gastrointestinal tract (GIT) using low methoxyl (LM) and high methoxy (HM) pectins and tetraethoxysilane (TEOS) as precursor is described. The FTIR spectra of the pectin-silica gels show intense absorption bands at 1246cm−1 and 802cm−1 corresponding to the vibrations COSi bonds, which absent in the FTIR spectra of the native pectins that indicate the formation covalent bond between silica and pectin macromolecules in the pectin-silica gels. Pectin-TEOS, pectin-Ca-TEOS and pectin-TEOS-Ca beads with mesalazine are synthesized by different combinations of sol-gel method using TEOS and ionotropic gelation method using calcium chloride. The best resistant of pectin-TEOS and pectin-Ca-TEOS beads during incubation in simulated gastric fluid for 2h and subsequently in simulated intestinal fluids for 18h is indicated. Pectin-TEOS beads are characterized by higher encapsulation efficiency (to 28%) than pectin-Ca-TEOS beads (to 16%). The drug release of pectin-silica beads in simulated GIT occurs gradually up to 80% and is directly dependent on the hardness of the beads. The surface morphology of beads is shown. The use of pectin-silica beads is promising with regard to the development of controlled release of drug formulations.